944696-30-4Relevant academic research and scientific papers
Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice
Purkey, Hans E.,Robarge, Kirk,Chen, Jinhua,Chen, Zhongguo,Corson, Laura B.,Ding, Charles Z.,Dipasquale, Antonio G.,Dragovich, Peter S.,Eigenbrot, Charles,Evangelista, Marie,Fauber, Benjamin P.,Gao, Zhenting,Ge, Hongxiu,Hitz, Anna,Ho, Qunh,Labadie, Sharada S.,Lai, Kwong Wah,Liu, Wenfeng,Liu, Yajing,Li, Chiho,Ma, Shuguang,Malek, Shiva,O'Brien, Thomas,Pang, Jodie,Peterson, David,Salphati, Laurent,Sideris, Steve,Ultsch, Mark,Wei, Binqing,Yen, Ivana,Yue, Qin,Zhang, Huihui,Zhou, Aihe
supporting information, p. 896 - 901 (2016/10/22)
A series of trisubstituted hydroxylactams was identified as potent enzymatic and cellular inhibitors of human lactate dehydrogenase A. Utilizing structure-based design and physical property optimization, multiple inhibitors were discovered with 50 in a MiaPaca2 cell line. Optimization of the series led to 29, a potent cell active molecule (MiaPaca2 IC50 = 0.67 μM) that also possessed good exposure when dosed orally to mice.
METHOD OF CONTROLLING LACTATE PRODUCTION WITH PIPERDINE-DIONE DERIVATIVES
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Page/Page column 78-79, (2015/11/10)
The invention provides novel compounds having the general formula: and tautomers and pharmaceutically acceptable salts thereof, wherein A1, A2, A3, A4, R1, R4, R5, R6, R7 and R8 are as defined herein, compositions including the compounds and methods of using the compounds.
PIPERIDINE-DIONE DERIVATIVES
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Page/Page column 89; 90, (2015/11/10)
The invention provides novel compounds having the general formula (I) and tautomers and pharmaceutically acceptable salts thereof, wherein A1, A2, A3, A4, R1, R4, R5, R6, R7 and R8 are as defined herein, compositions including the compounds and methods of using the compounds.
CATHEPSIN CYSTEINE PROTEASE INHIBITORS
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Page 56, (2010/02/06)
This invention relates to class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis. They have the following structure: Formula (I).
